52130-34-4Relevant academic research and scientific papers
Derivatives of (R)-3-(5-Furanyl)carboxamido-2-aminopropanoic Acid as Potent NMDA Receptor Glycine Site Agonists with GluN2 Subunit-Specific Activity
Zhao, Fabao,Atxabal, Unai,Mariottini, Sofia,Yi, Feng,Lotti, James S.,Rouzbeh, Nirvan,Liu, Na,Bunch, Lennart,Hansen, Kasper B.,Clausen, Rasmus P.
, p. 734 - 746 (2022/01/03)
NMDA receptors mediate glutamatergic neurotransmission and are therapeutic targets due to their involvement in a variety of psychiatric and neurological disorders. Here, we describe the design and synthesis of a series of (R)-3-(5-furanyl)carboxamido-2-am
Multicomponent one pot synthesis and characterization of novel 4-furyl-1,4-dihydropyridines
Zafar, Ansa Madeeha,Aslam, Samina,Khakwani, Samia,Khan, Muhammad Naeem,Munawar, Munawar Ali,Khan, Misbahul Ain
, p. 735 - 741 (2017/02/10)
A series of dihydropyridines were prepared from the multi-component reaction of 5-arylfuran-2-carbaldehydes, ethylacetoacetate and ammonium acetate. These compounds were characterized through elemental analysis and various spectroscopic techniques (FTIR, 1H NMR, 13C NMR and mass).
Discovery of selective protein arginine methyltransferase 5 inhibitors and biological evaluations
Ji, Sen,Ma, Shuang,Wang, Wen-Jing,Huang, Shen-Zhen,Wang, Tian-Qi,Xiang, Rong,Hu, Yi-Guo,Chen, Qiang,Li, Lin-Li,Yang, Sheng-Yong
, p. 585 - 598 (2017/04/06)
Protein arginine methyltransferase 5 (PRMT5) is an important protein arginine methyltransferase that catalyzes the symmetric dimethylation of arginine resides on histones or non-histone substrate proteins. It has been thought as a promising target for many diseases, particularly cancer. Despite the potential applications of PRMT5 inhibitors in cancer treatment, very few of PRMT5i have been publicly reported. In this investigation, virtual screening and structure–activity relationship studies were carried out to discover novel PRMT5i, which finally led to the identification of a number of new PRMT5i. The most active compound, P5i-6, exhibited a considerable inhibitory potency against PRMT5 with an IC50 value of 0.57?μm, and a high selectivity for PRMT5 against other tested PRMTs. It displayed a very good antiviability activity against two colorectal cancer cell lines, HT-29 and DLD-1, and one hepatic cancer cell line, HepG2, in a sensitivity assay against 36 different cancer cell lines. Western blot assays indicated that P5i-6 selectively inhibited the symmetric dimethylations of H4R3 and H3R8 in DLD-1 cells. Overall, P5i-6 could be used as a chemical probe to investigate new functions of PRMT5 in biology and also served as a good lead compound for the development of new PRMT5-targeting therapeutic agents.
Novel inhibitors of Plasmodium falciparum based on 2,5-disubstituted furans
Krake, Susann H.,Martinez, Pablo David G.,McLaren, Jenna,Ryan, Eileen,Chen, Gong,White, Karen,Charman, Susan A.,Campbell, Simon,Willis, Paul,Dias, Luiz Carlos
supporting information, p. 929 - 936 (2016/12/23)
Phenotypic HTS campaigns with a blood stage malaria assay have been used to discover novel chemotypes for malaria treatment with potential alternative mechanisms of action compared to existing agents. N1-(5-(3-Chloro-4-fluorophenyl)furan-2-yl)-N3,N3-dimethylpropane-1,3-diamine, 1 was identified as a modest inhibitor of P. falciparum NF54 (IC50= 875 nM) with an apparent long plasma half-life after high dose oral administration to mice, although the compound later showed poor metabolic stability in liver microsomes through ring- and side chain-oxidation and N-dealkylation. We describe here the synthesis of derivatives of 1, exploring the influence of substitution patterns around the aromatic ring, variations on the alkyl chain and modifications in the core heterocycle, in order to probe potency and metabolic stability, where 4k showed a long half-life in rats.
Identification of a small molecule inhibitor that stalls splicing at an early step of spliceosome activation
Sidarovich, Anzhalika,Will, Cindy L.,Anokhina, Maria M.,Ceballos, Javier,Sievers, Sonja,Agafonov, Dmitry E.,Samatov, Timur,Bao, Penghui,Kastner, Berthold,Urlaub, Henning,Waldmann, Herbert,Lührmann, Reinhard
, (2017/03/23)
Small molecule inhibitors of pre-mRNA splicing are important tools for identifying new spliceosome assembly intermediates, allowing a finer dissection of spliceosome dynamics and function. Here, we identified a small molecule that inhibits human pre-mRNA splicing at an intermediate stage during conversion of pre-catalytic spliceosomal B complexes into activated Bact complexes. Characterization of the stalled complexes (designated B028) revealed that U4/U6 snRNP proteins are released during activation before the U6 Lsm and B-specific proteins, and before recruitment and/or stable incorporation of Prp19/CDC5L complex and other Bact complex proteins. The U2/U6 RNA network in B028 complexes differs from that of the Bact complex, consistent with the idea that the catalytic RNA core forms stepwise during the B to Bact transition and is likely stabilized by the Prp19/CDC5L complex and related proteins. Taken together, our data provide new insights into the RNP rearrangements and extensive exchange of proteins that occurs during spliceosome activation.
A HIGH-THROUGHPUT ASSAY FOR IDENTIFYING SMALL MOLECULES THAT MODULATE AMP-ACTIVATED PROTEIN KINASE (AMPK)
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Page/Page column 63; 64, (2016/02/29)
The present invention provides an in vitro method for identifying a compound that modulates adenosine monophosphate-activated protein kinase (AMPK) for the manufacture of a diagnostic or therapeutic agent. The present invention further provides an assay for identifying a compound that modulates AMPK.
Synthesis and biological evaluation of chalcones and acetyl pyrazoline derivatives comprising furan nucleus as an antitubercular agents
Bhoot, Dinesh,Khunt, Ranjan C.,Parekh, Hansa H.
, p. 3233 - 3239 (2012/10/29)
A series of 1-{5-[5-(m,p-dichlorophenyl)furan- 2-yl]-3-aryl-4,5-dihydro-1H- pyrazol-1-yl} ethanone (3a-k) have been synthesized by the condensation of (2E)- 3-[5-(m,p-dichlorophenyl)furan-2-yl]-1-arylprop-2-en-1-one (2a-k) with hydrazine hydrate in glacia
Investigation of N-aryl-3-alkylidenepyrrolinones as potential Niemann-Pick type C disease therapeutics
Cosner, Casey C.,Markiewicz, John T.,Bourbon, Pauline,Mariani, Christopher J.,Wiest, Olaf,Rujoi, Madalina,Rosenbaum, Anton I.,Huang, Amy Y.,Maxfield, Frederick R.,Helquist, Paul
supporting information; experimental part, p. 6494 - 6498 (2010/03/31)
A five-step synthesis of an array of N-aryl-3-alkylidenepyrrolinones, which are potential Niemann-Pick type C (NPC) disease therapeutics, is described. The synthetic route allows for the production of analogues, including photoaffinity and biotinylated de
Methods for treating viral infections
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, (2008/06/13)
Methods are provided for the treatment and prophylaxis of viral infection and disease associated with such infection.
Compounds, compositions and methods for treating or preventing viral infections and associated diseases
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, (2008/06/13)
Compounds, compositions and methods are provided for the treatment and prophylaxis of infections and associated diseases caused by viruses of the Flaviviridae family by administering certain rhodanine derivatives, and analogs thereof, tri- and tetracyclic
